[BRL 43694A--a 5-hydroxytryptamine receptor blocker as an antiemetic in cytostatic therapy]

An open study of the new antiemetic BRL 43694A, a 5-hydroxytryptamine-3-receptor antagonist, was performed in 29 patients undergoing highly emetogenic cancer chemotherapy (25 patients received cisplatin in a dose greater than or equal to 50 mg/m2). Patients received BRL 43694A as a 30-minute infusion one hour after the administration of chemotherapy. 7 patients were treated with 40 micrograms/kg and 13 patients with 100 micrograms/kg BRL 43694A; the last 9 patients received an initial dose of 40 micrograms/kg with a provision for two additional interventional doses over 24 hours in the event of prolonged nausea or vomiting. 14 patients experienced no vomiting (48%) and 13 patients (45%) had 1-5 vomiting episodes over 24 hours following administration of the cytostatic agents. BRL 43694A did not cause major side effects. Based on our preliminary experience the new 5-HT3-receptor antagonist BRL 43694A is a potent antiemetic drug for the treatment of chemotherapy-induced nausea and vomiting.